PE20060317A1 - XANTINE DERIVATIVES AS SELECTIVE AGONISTS OF THE NICOTINIC ACID RECEPTOR - Google Patents

XANTINE DERIVATIVES AS SELECTIVE AGONISTS OF THE NICOTINIC ACID RECEPTOR

Info

Publication number
PE20060317A1
PE20060317A1 PE2005000170A PE2005000170A PE20060317A1 PE 20060317 A1 PE20060317 A1 PE 20060317A1 PE 2005000170 A PE2005000170 A PE 2005000170A PE 2005000170 A PE2005000170 A PE 2005000170A PE 20060317 A1 PE20060317 A1 PE 20060317A1
Authority
PE
Peru
Prior art keywords
nicotinic acid
acid receptor
selective agonists
alkyl
diona
Prior art date
Application number
PE2005000170A
Other languages
Spanish (es)
Inventor
Ivan Leo Pinto
Shahzad Sharooq Rahman
Neville Hubert Nicholson
Original Assignee
Smithkline Beecham Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB0403282A external-priority patent/GB0403282D0/en
Priority claimed from GB0423562A external-priority patent/GB0423562D0/en
Priority claimed from GB0428375A external-priority patent/GB0428375D0/en
Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of PE20060317A1 publication Critical patent/PE20060317A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE R1 H, ALQUILO C1-C4 SUSTITUIDO O NO POR CN, CF3; R2 ES ALQUILO C3-C10, ALQUILO C1-C10 SUSTITUIDO CON 1 O MAS GRUPOS DE F, CN, ENTRE OTROS; R3 ES HALOGENO, CN. SON COMPUESTOS PREFERIDOS: 8-CLORO-3-(4-PENTEN-1-IL)-3,7-DIHIDRO-1H-PURINA-2,6-DIONA; (8-CLORO-2,6-DIOXO-1,2,6,7-TETRAHIDRO-3H-PRIN-3-IL)ACETONITRILO; 8-CLORO-3-(4,4,4-TRIFLUOROBUTIL)-3,7-DIHIDRO-1H-PURINA-2,6-DIONA; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON AGONISTAS SELECTIVOS DEL RECEPTOR DE ACIDO NICOTINICO HM74A UTILES EN ENFERMEDADES DEL METABOLISMO DE LIPIDOS, INSUFICIENCIA CARDIACA, ARTERIOSCLEROSIS, TROMBOSIS, ANGINA, ENTRE OTROSREFERS TO A COMPOUND OF FORMULA I, WHERE R1 H, C1-C4 ALKYL SUBSTITUTE OR NOT BY CN, CF3; R2 IS C3-C10 ALKYL, C1-C10 ALKYL SUBSTITUTED WITH 1 OR MORE GROUPS OF F, CN, AMONG OTHERS; R3 IS HALOGEN, CN. PREFERRED COMPOUNDS ARE: 8-CHLORINE-3- (4-PENTEN-1-IL) -3,7-DIHYDRO-1H-PURINE-2,6-DIONA; (8-CHLORO-2,6-DIOXO-1,2,6,7-TETRAHYDRO-3H-PRIN-3-IL) ACETONITRILE; 8-CHLORO-3- (4,4,4-TRIFLUOROBUTIL) -3,7-DIHYDRO-1H-PURINE-2,6-DIONA; AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION AND A PREPARATION PROCEDURE. SUCH COMPOUNDS ARE SELECTIVE AGONISTS OF THE HM74A NICOTINIC ACID RECEPTOR USEFUL IN DISEASES OF LIPID METABOLISM, HEART FAILURE, ARTERIOSCLEROSIS, THROMBOSIS, ANGINA, AMONG OTHERS

PE2005000170A 2004-02-14 2005-02-11 XANTINE DERIVATIVES AS SELECTIVE AGONISTS OF THE NICOTINIC ACID RECEPTOR PE20060317A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0403282A GB0403282D0 (en) 2004-02-14 2004-02-14 Chemical compounds
GB0423562A GB0423562D0 (en) 2004-10-22 2004-10-22 Novel compounds
GB0428375A GB0428375D0 (en) 2004-12-24 2004-12-24 Novel compounds

Publications (1)

Publication Number Publication Date
PE20060317A1 true PE20060317A1 (en) 2006-06-22

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005000170A PE20060317A1 (en) 2004-02-14 2005-02-11 XANTINE DERIVATIVES AS SELECTIVE AGONISTS OF THE NICOTINIC ACID RECEPTOR

Country Status (26)

Country Link
US (5) US7713982B2 (en)
EP (1) EP1781657B1 (en)
JP (2) JP5001012B2 (en)
KR (1) KR101100601B1 (en)
CN (2) CN101863888B (en)
AR (1) AR047669A1 (en)
AU (1) AU2005212816C1 (en)
BR (1) BRPI0507604A (en)
CA (1) CA2556073C (en)
CY (1) CY1114022T1 (en)
DK (1) DK1781657T3 (en)
ES (1) ES2406732T3 (en)
HK (1) HK1104530A1 (en)
HR (1) HRP20130406T1 (en)
IL (1) IL177051A (en)
MA (1) MA28357A1 (en)
MY (1) MY148937A (en)
NO (1) NO337281B1 (en)
NZ (1) NZ548496A (en)
PE (1) PE20060317A1 (en)
PL (1) PL1781657T3 (en)
PT (1) PT1781657E (en)
SG (1) SG157242A1 (en)
SI (1) SI1781657T1 (en)
TW (1) TWI350289B (en)
WO (1) WO2005077950A2 (en)

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Publication number Publication date
AU2005212816C1 (en) 2010-03-04
CN101103030B (en) 2010-10-13
PL1781657T3 (en) 2013-08-30
AR047669A1 (en) 2006-02-01
TW200536537A (en) 2005-11-16
US20100160354A1 (en) 2010-06-24
US20150080418A1 (en) 2015-03-19
IL177051A (en) 2013-01-31
JP5020848B2 (en) 2012-09-05
MY148937A (en) 2013-06-14
ES2406732T3 (en) 2013-06-07
CN101863888A (en) 2010-10-20
US20130150383A1 (en) 2013-06-13
IL177051A0 (en) 2006-12-10
AU2005212816B2 (en) 2009-07-23
NO20064151L (en) 2006-11-06
SG157242A1 (en) 2009-12-29
WO2005077950A3 (en) 2007-04-19
CA2556073C (en) 2012-01-10
CN101863888B (en) 2012-07-18
MA28357A1 (en) 2006-12-01
US20100010021A1 (en) 2010-01-14
BRPI0507604A (en) 2007-07-03
EP1781657B1 (en) 2013-03-27
WO2005077950A2 (en) 2005-08-25
HK1104530A1 (en) 2008-01-18
HRP20130406T1 (en) 2013-06-30
AU2005212816A1 (en) 2005-08-25
US8394808B2 (en) 2013-03-12
CY1114022T1 (en) 2016-07-27
TWI350289B (en) 2011-10-11
JP5001012B2 (en) 2012-08-15
PT1781657E (en) 2013-05-23
KR20060126772A (en) 2006-12-08
CN101103030A (en) 2008-01-09
US8268839B2 (en) 2012-09-18
JP2008120831A (en) 2008-05-29
JP2007522176A (en) 2007-08-09
CA2556073A1 (en) 2005-08-25
EP1781657A2 (en) 2007-05-09
NZ548496A (en) 2010-02-26
KR101100601B1 (en) 2011-12-29
US7713982B2 (en) 2010-05-11
DK1781657T3 (en) 2013-06-10
NO337281B1 (en) 2016-02-29
US20070135456A1 (en) 2007-06-14
SI1781657T1 (en) 2013-07-31

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